Material Data Sheet
Potent, highly specific, irreversible and cell-permeable inhibitor that covalently modifies the catalytic β subunits (chymotrypsin-, trypsin- and caspase-like activities) of the proteasome. Lactacystin is hydrolyzed in aqueous solutions to a clasto-lactacystin β-lactone intermediate which is the active inhibitory species that reacts with the proteasome.
Purity:> 98% by HPLC. Structure confirmed by H-NMR.
Solubility:Soluble and stable in DMSO or MeCN up to 20 mg/ml. Pellet dry compound prior to DMSO addition. Subject to hydrolysis in aqueous buffers.
kobs/[I] = 4,000 M-1 s-1 vs. 20S:PA28 complex.
Inhibits ubiquitin proteasome pathway in cell culture (IC50=10 μM).
Store at -20°C. Avoid multiple freeze/thaw cycles.
Dick R.L., et al. (1996) J. Biol. Chem. 271:7273-7276
Dick R.L., et al. (1997) J. Biol. Chem. 272:182-188
Craiu A., et al. (1997) J. Biol. Chem. 272:13437-13445
Fenteany G. and Schreiber S.L. (1998) J. Biol. Chem. 273:8545-8548
Fenteany G et al. (1995) Science. 268:726-731
Masse C.E., et al. (2000) Eur. J. Org. Chem. 714:2513-2528